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公开(公告)号：US07960415B2
公开(公告)日：2011-06-14
申请号：US12140497
申请日：2008-06-17
申请人： Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Michael Mortimore , John Studley
发明人： Guy Brenchley , Jean-Damien Charrier , Steven Durrant , Ronald Knegtel , Michael Mortimore , John Studley
IPC分类号： A61K31/44 , C07D211/72
CPC分类号： C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
摘要： The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
摘要翻译： 本发明提供式I化合物：其中R 1，R 2，R 3，R 4和R 5如本文所定义。 本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病的药物组合物和方法以及制备本发明化合物的方法。
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公开(公告)号：US07951820B2
公开(公告)日：2011-05-31
申请号：US11492450
申请日：2006-07-25
申请人： David Bebbington , Ronald Knegtel , Hayley Binch , Julian M. C. Golec , Pan Li , Jean-Damien Charrier
发明人： David Bebbington , Ronald Knegtel , Hayley Binch , Julian M. C. Golec , Pan Li , Jean-Damien Charrier
IPC分类号： A01N43/42 , A61K31/47 , A01N43/40 , A61K31/44 , C07D217/22 , C07D217/00 , C07D215/38 , C07D213/72
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T-R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; R1, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of GSK-3 and Aurora, for treating diseases such as diabetes, cancer, and Alzheimer's disease.
摘要翻译： 本发明描述了式IX的新型三唑化合物：其中Z1是氮或CR9，Z2是氮或CH，条件是Z1和Z2中的至少一个是氮; G是环C或环D; 环C选自苯基，吡啶基，嘧啶基，哒嗪基，吡嗪基或1,2,4-三嗪基，其中所述环C具有一个或两个独立地选自-R 1的邻位取代基; 环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; Rx和Ry独立地选自T-R3，或Rx和Ry与它们的插入原子一起形成稠环; R1，R3和T如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为GSK-3和Aurora的抑制剂，用于治疗诸如糖尿病，癌症和阿尔茨海默病的疾病。
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公开(公告)号：US20110021519A1
公开(公告)日：2011-01-27
申请号：US12796174
申请日：2010-06-08
申请人： Jean-Damien Charrier , David Kay , Ronald Knegtel
发明人： Jean-Damien Charrier , David Kay , Ronald Knegtel
IPC分类号： A61K31/5377 , C07D487/12 , A61K31/519 , C07D413/14 , A61P35/00 , A61P37/06 , A61P19/08 , A61P3/00 , A61P25/00 , A61P9/00 , A61P5/00
CPC分类号： C07D487/14
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US07838517B2
公开(公告)日：2010-11-23
申请号：US12466420
申请日：2009-05-15
IPC分类号： C07D495/04 , C07D513/04 , C07D519/00 , A61K31/4188 , A61K31/4184 , A61K31/55
CPC分类号： C07D513/04 , A61K31/55 , A61K31/551 , A61K45/06 , C07D495/04 , C07D519/00 , C07K14/81
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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![5-CYANO-4- (PYRROLO [2,3] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS](/abs-image/US/2010/07/29/US20100189773A1/abs.jpg.150x150.jpg)
55.发明申请5-CYANO-4- (PYRROLO [2,3] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS 失效用作蛋白激酶抑制剂的5-氰基-4-（吡咯并[2,3]吡啶-3-基） - 吡啶衍生物公开(公告)号：US20100189773A1
公开(公告)日：2010-07-29
申请号：US12448489
申请日：2007-12-21
申请人： Michael Mortimore , Stephen Clinton Young , Simon Robert Lorrie Everitt , Ronald Knegtel , Joanne Louise Pinder , Alistair Peter Rutherford , Steven Durrant , Guy Brenchley , Jean-Damien Charrier , Michael O'Donnell
发明人： Michael Mortimore , Stephen Clinton Young , Simon Robert Lorrie Everitt , Ronald Knegtel , Joanne Louise Pinder , Alistair Peter Rutherford , Steven Durrant , Guy Brenchley , Jean-Damien Charrier , Michael O'Donnell
IPC分类号： A61K9/127 , C07D487/04 , A61K31/506 , A61K31/5377 , A61K31/551 , A61P35/00 , A61P3/10 , A61P7/00 , A61P19/02 , A61P37/00 , A61P35/02 , A61K38/50 , A61K31/565 , A61K38/19 , A61K39/395 , A61K31/7088 , A61K31/661 , A61K33/24 , A61K31/7008 , A61K31/704 , A61K31/7068 , A61K31/69 , A61K38/21 , A61K38/20 , C12N5/00
CPC分类号： C07D471/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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公开(公告)号：US07622463B2
公开(公告)日：2009-11-24
申请号：US11706070
申请日：2007-02-13
申请人： David Kay , Ronald Knegtel , Jean-Damien Charrier , Heather Twin
发明人： David Kay , Ronald Knegtel , Jean-Damien Charrier , Heather Twin
IPC分类号： C07D401/12 , A61K31/4545
CPC分类号： C07D487/04 , A61K31/551 , A61K45/06 , C07D487/14
摘要： The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译： 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。
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57.发明授权Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors 有权用作蛋白激酶抑制剂的吡唑啉胺取代喹唑啉化合物公开(公告)号：US07098330B2
公开(公告)日：2006-08-29
申请号：US09952878
申请日：2001-09-14
申请人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian M. C. Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert J. Davies
发明人： David Bebbington , Hayley Binch , Ronald Knegtel , Julian M. C. Golec , Sanjay Patel , Jean-Damien Charrier , David Kay , Robert J. Davies
IPC分类号： C07D401/14 , C07D403/12 , C07D405/04 , A61K31/517
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are taken together with their intervening atoms to form a fused, unsaturated or partially unsaturated, 5–8 membered carbocyclo ring; and R2 and R2′ are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
摘要翻译： 本发明描述了式III的新型吡唑化合物：其中环D是选自芳基，杂芳基，杂环基或碳环基的5-7元单环或8-10元双环; R x和R y与它们的插入原子一起形成稠合的，不饱和的或部分不饱和的5-8元碳环; 和R 2和R 2'如说明书中所述。 这些化合物可用作蛋白激酶抑制剂，特别是作为用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病的极光-2和GSK-3的抑制剂。
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公开(公告)号：US07091343B2
公开(公告)日：2006-08-15
申请号：US10389296
申请日：2003-03-14
申请人： David Bebbington , Hayley Binch , Jean-Damien Charrier , Simon Everitt , Julian M. C. Golec , David Kay , Ronald Knegtel , Andrew Miller , Francoise Pierard
发明人： David Bebbington , Hayley Binch , Jean-Damien Charrier , Simon Everitt , Julian M. C. Golec , David Kay , Ronald Knegtel , Andrew Miller , Francoise Pierard
IPC分类号： C07D403/12 , C07D409/14 , C07D417/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译： 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。
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公开(公告)号：US20060160862A1
公开(公告)日：2006-07-20
申请号：US11284366
申请日：2005-11-21
IPC分类号： A61K31/4439 , A61K31/4412 , C07D401/02 , C07D211/72
CPC分类号： C07D213/75 , C07D211/72 , C07D401/02 , C07D401/06 , C07D409/06
摘要： The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparting the compounds of the invention.
摘要翻译： 本发明提供式I化合物：其中R 1，R 2，R 3，R 4， R 5和R 5如本文所定义。 本发明还提供了使用这样的组合物治疗半胱天冬酶介导的疾病的药物组合物和方法以及用于制备本发明化合物的方法。
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公开(公告)号：US07053057B2
公开(公告)日：2006-05-30
申请号：US09863649
申请日：2001-05-23
CPC分类号： C07D401/12 , C07D211/60 , C07D215/48 , C07D409/12
摘要： This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.
摘要翻译： 本发明提供了具有下式的半胱天冬酶抑制剂：其中环A是任选取代的哌啶，四氢喹啉或四氢异喹啉环; R 1是氢，CHN 2，R或-CH 2 Y; R是选自脂族基团，芳基，芳烷基，杂环基或杂环基烷基的任选取代的基团; Y是电负离子团; R 2是CO 2 H，CH 2 CO 2 H，或它们的酯，酰胺或等体醇; Ar是任选取代的芳基; 和R 3是氢，任选取代的C 1-6烷基，F 2，CN，芳基或R 3， SUP>与Ar连接形成不饱和或部分饱和的具有0-2个杂原子的五元或六元稠环。 该化合物可用于治疗哺乳动物中半胱天冬酶介导的疾病。
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